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Literature summary for 3.4.21.98 extracted from

  • Bailey, M.D.; Halmos, T.; Goudreau, N.; Lescop, E.; Llinas-Brunet, M.
    Novel azapeptide inhibitors of hepatitis C virus serine protease (2004), J. Med. Chem., 47, 3788-3799.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-([(1S)-1-(4-bromophenyl)ethyl]carbamoyl)-2-propylhydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid noncovalent binding to enzyme active site, 50% inhibition at 0.000072 mM Hepacivirus C
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-([(1S)-2,3-dihydro-1H-inden-1-yl]carbamoyl)-2-propylhydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid noncovalent binding to enzyme active site, 50% inhibition at 0.0001 mM Hepacivirus C
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-butyl-2-([(1S)-1-phenylethyl]carbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid noncovalent binding to enzyme active site, 50% inhibition at 0.000099 mM, over 400fold selectivity for enzyme over human leukocyte elastase Hepacivirus C
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2S,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-ethyl-2-([(1S)-1-phenylethyl]carbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid noncovalent binding to enzyme active site, 50% inhibition at 0.000085 mM Hepacivirus C
(4R)-4-[[(2S)-2-(acetylamino)-3-carboxypropanoyl]amino]-5-[(1-[[(1R)-1-([(2S,4R)-4-(benzyloxy)-2-[(2-[[(1S)-1-phenylethyl]carbamoyl]-2-propylhydrazino)carbonyl]pyrrolidin-1-yl]carbonyl)-2-methylpropyl]carbamoyl]-2-methylbutyl)amino]-5-oxopentanoic acid noncovalent binding to enzyme active site, 50% inhibition at 0.000078 mM Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
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